Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists

被引：17
|
作者：
Xiao, Yufang [1 ]
Araldi, Gian Luca
Zhao, Zhong
Brugger, Nadia
Karra, Srinivasa
Fischer, David
Palmer, Elizabeth
机构：
[1] EMD Serono Res Inst Inc, Dept Med Chem, Rockland, MA 02370 USA
[2] EMD Serono Res Inst Inc, Dept Lead Discovery, Rockland, MA 02370 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 15期
关键词：
prostaglandin; PROSTANOID RECEPTORS; STEREOSELECTIVE HYDROGENOLYSIS; STEREOSPECIFIC SYNTHESIS; KNOCKOUT MICE; ACID; (Z)-1-BROMO-1-ALKENES; 1,1-DIBROMO-1-ALKENES; SUBTYPES;
D O I：
10.1016/j.bmcl.2007.05.025
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Analogs of PGE(2) with introduction of diene groups at the co-side chain have been synthesized and evaluated for their binding affinity for EP2 and EP4 receptors. An optimized analog (compound 9b) showed high potency and selectivity for the EP4 receptor over other known receptors. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4323 / 4327
页数：5
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